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Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility

A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmen...

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Autores principales: Friuli, Valeria, Pisani, Silvia, Conti, Bice, Bruni, Giovanna, Maggi, Lauretta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9142934/
https://www.ncbi.nlm.nih.gov/pubmed/35632009
http://dx.doi.org/10.3390/polym14102127
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author Friuli, Valeria
Pisani, Silvia
Conti, Bice
Bruni, Giovanna
Maggi, Lauretta
author_facet Friuli, Valeria
Pisani, Silvia
Conti, Bice
Bruni, Giovanna
Maggi, Lauretta
author_sort Friuli, Valeria
collection PubMed
description A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances.
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spelling pubmed-91429342022-05-29 Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility Friuli, Valeria Pisani, Silvia Conti, Bice Bruni, Giovanna Maggi, Lauretta Polymers (Basel) Article A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances. MDPI 2022-05-23 /pmc/articles/PMC9142934/ /pubmed/35632009 http://dx.doi.org/10.3390/polym14102127 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Friuli, Valeria
Pisani, Silvia
Conti, Bice
Bruni, Giovanna
Maggi, Lauretta
Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
title Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
title_full Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
title_fullStr Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
title_full_unstemmed Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
title_short Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility
title_sort tablet formulations of polymeric electrospun fibers for the controlled release of drugs with ph-dependent solubility
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9142934/
https://www.ncbi.nlm.nih.gov/pubmed/35632009
http://dx.doi.org/10.3390/polym14102127
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